公开(公告)号：US09469647B2

公开(公告)日：2016-10-18

申请号：US14409988

申请日：2013-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Lawrence P. Wennogle ,  Robert Davis ,  Graham Buckton ,  Mark Hooper

IPC: C07D487/14 ,  A61K31/519 ,  A61P35/00 ,  C07C55/02 ,  C07C57/15 ,  C07C309/04

CPC classification number: C07D487/14 ,  C07B2200/13 ,  C07C55/02 ,  C07C57/15 ,  C07C309/04

Abstract: The present invention relates to acid addition salt and salt crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, composition comprising the same and the method of making and using such salt and crystal.

Abstract translation: 本发明涉及（6aR，9aS）-5,6a，7,8,9,9a-六氢-5-甲基-3-（苯基氨基）-2 - （（4-（6 - 氟吡啶-2-基）苯基）甲基） - 环戊并[4,5]咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（2H） - 酮，包含该组合物的组合物和方法 制作和使用这种盐和水晶。

公开(公告)号：US20150079172A1

公开(公告)日：2015-03-19

申请号：US14394467

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Peng Li ,  Lawrence Wennogle ,  Richard A. Lerner

IPC: C07D471/14

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/16 ,  A61K2300/00

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.

Abstract translation: 本发明涉及如本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式的特定取代的杂环稠合的γ-咔啉及其前药，其药物组合物，以及用于治疗涉及5-HT2A 受体，血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径。

公开(公告)号：US12240850B2

公开(公告)日：2025-03-04

申请号：US18314785

申请日：2023-05-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/437 ,  A61K9/48 ,  A61K9/50 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22

Abstract: The invention relates to pharmaceutical compositions comprising compounds of Formula Q: wherein W is —N(CH3)—, and Y is —CH(OH)—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

公开(公告)号：US12195462B2

公开(公告)日：2025-01-14

申请号：US17415565

申请日：2019-12-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis

IPC: C07D471/16 ,  A61K9/16

Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or pharmaceutically acceptable salt, and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), and/or pathways involving the dopamine D1 and D2 receptor signaling system.

公开(公告)号：US12023331B2

公开(公告)日：2024-07-02

申请号：US17115416

申请日：2020-12-08

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen Snyder ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  A61K45/06 ,  A61P25/22 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61P25/22 ,  A61P25/24 ,  A61K45/06

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A/mu-opioid receptor or 5-HT2A/D1 and/or D2/mu-opioid receptor ligand.

公开(公告)号：US11844757B2

公开(公告)日：2023-12-19

申请号：US17015883

申请日：2020-09-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61P25/00 ,  A61K45/00 ,  A61K45/06 ,  C07D471/16 ,  A61K9/00 ,  A61K9/16 ,  C07D241/40 ,  A61K31/445

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/16 ,  A61K31/445 ,  A61K45/00 ,  A61K45/06 ,  A61P25/00 ,  C07D241/40 ,  C07D471/16

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US11759465B2

公开(公告)日：2023-09-19

申请号：US16892206

申请日：2020-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David Kass ,  Toru Hashimoto ,  Lawrence P. Wennogle ,  Joseph Hendrick ,  Robert Davis

IPC: A61K31/519 ,  A61P9/04 ,  A61K31/197 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/7056 ,  A61K9/00 ,  A61K45/06

CPC classification number: A61K31/519 ,  A61K9/0053 ,  A61K31/197 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/7056 ,  A61K45/06 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

公开(公告)号：US11560382B2

公开(公告)日：2023-01-24

申请号：US17124224

申请日：2020-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Peng Li ,  Lawrence P. Wennogle ,  Robert Davis

IPC: C07D471/16 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  A61K45/06 ,  C07D471/14 ,  C07B59/00 ,  A61K31/4985

Abstract: This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

公开(公告)号：US11124514B2

公开(公告)日：2021-09-21

申请号：US16585251

申请日：2019-09-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover ,  Lawrence Wennogle

IPC: A61K31/50 ,  A61K31/13 ,  A61K31/445 ,  A61K31/44 ,  A61K31/27 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  A61P25/28 ,  C07D471/16

Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.

公开(公告)号：US10799500B2

公开(公告)日：2020-10-13

申请号：US16276331

申请日：2019-02-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  C07D471/16 ,  C07D241/40 ,  A61K31/445 ,  A61P25/00 ,  A61K9/00 ,  A61K9/16 ,  A61K45/00 ,  A61K45/06

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.